Description
p-nitro-Pifithrin-α, a cell-permeable cyclic analog of pifithrin-α, is an inhibitor of p53 activity . The p53 tumor suppressor gene product can induce apoptotic cell death and plays a dominant role in apoptosis, genomic stability, and inhibition of angiogenesis. The p53 has been considered to be an oncogene and the wild-type gene product actually functions as a tumour suppressor gene. p53 mutations play an important role in the development of many common human malignancies . In Vitro: In p53-/- cortical neuron, p-nitro-Pifithrin-α exihibited a p53 inhibitory activity in preventing p53-induced death. p-nitro-Pifithrin-α did not prevent cortical neuronal death induced by p40Met, showing the remarkable specificity in the inhibitory action of p-nitro-Pifithrin-α on p53. p-nitro-Pifithrin-α (300 nM) prevented p53-triggered increase in protein levels of p21/WAF1, indicating that p-nitro-Pifithrin-α behaved as p53 posttranscriptional activity inhibitors. p-nitro-Pifithrin-α at a dose of 30 nM was sufficient to prevent the increase of p21/WAF1 levels . p-nitro-Pifithrin-α was slowly converted into a more potent cyclized form, p-nitro cyclic pifithrin-α, when incubated in biological media (t1/2= 8 h) In human proximal tubular cells, p-nitro-Pifithrin-α (10 μM) suppressed p53-mediated TGF-β1 expression . In vivo: In a mouse model of non-alcoholic fatty liver disease, p-nitro-Pifithrin-α attenuated steatosis and liver injury in mice fed a high-fat diet .
Product information
CAS Number: 389850-21-9
Molecular Weight: 398.27
Formula: C15H16BrN3O3S
Chemical Name: 2-(2-imino-2,3,4,5,6,7-hexahydro-1,3-benzothiazol-3-yl)-1-(4-nitrophenyl)ethan-1-one hydrobromide
Smiles: Br.N=C1SC2CCCCC=2N1CC(=O)C1C=CC(=CC=1)[N+]([O-])=O
InChiKey: NXPCMOGORSWOLH-UHFFFAOYSA-N
InChi: InChI=1S/C15H15N3O3S.BrH/c16-15-17(12-3-1-2-4-14(12)22-15)9-13(19)10-5-7-11(8-6-10)18(20)21;/h5-8,16H,1-4,9H2;1H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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